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Bioorg Med Chem Lett. 2008 Jan 15;18(2):629-33. Epub 2007 Nov 28.

Development of CXCR3 antagonists. Part 4: discovery of 2-amino-(4-tropinyl)quinolines.

Author information

1
UCB Inflammation Discovery, Granta Park, Great Abington, Cambridge CB21 6GS, United Kingdom. roland.knight@ucb-group.com

Abstract

The synthesis and biological evaluation of a novel series of 2-aminoquinoline substituted piperidines and tropanes incorporating a homotropene moiety is herein described. The series exhibits potent antagonism of the CXCR3 receptor and superior physicochemical properties. Compound 24d was found to be orally bioavailable, and PK/PD studies suggested it as a suitable tool for studying the role of CXCR3 in models of disease.

PMID:
18068363
DOI:
10.1016/j.bmcl.2007.11.075
[Indexed for MEDLINE]

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